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用于胰腺神经内分泌肿瘤成像的放射性药物的现状与最新进展

State of the Art and Recent Developments of Radiopharmaceuticals for Pancreatic Neuroendocrine Tumors Imaging.

作者信息

Carollo Angela, Papi Stefano, Grana Chiara M, Mansi Luigi, Chinol Marco

机构信息

Division of Nuclear Medicine, European Institute of Oncology Via Ripamonti 435 20141 Milano, Italy.

Section Health and Development, Interuniversity Research Center for Sustainability (CIRPS), Napoli, Italy.

出版信息

Curr Radiopharm. 2019;12(2):107-125. doi: 10.2174/1874471012666190306104450.

Abstract

BACKGROUND

Neuroendocrine Tumors (NETs) are relatively rare tumors, mainly originating from the digestive system, that tend to grow slowly and are often diagnosed when metastasised. Surgery is the sole curative option but is feasible only in a minority of patients. Among them, pancreatic neuroendocrine tumors (pancreatic NETs or pNETs) account for less than 5% of all pancreatic tumors. Viable therapeutic options include medical treatments such as biotherapies and more recently Peptide Receptor Radionuclide Therapies (PRRT) with radiolabeled somatostatin analogues. Molecular imaging, with main reference to PET/CT, has a major role in patients with pNETs.

OBJECTIVE

The overexpression of specific membrane receptors, as well as the ability of cells to take up amine precursors in NET, have been exploited for the development of specific targeting imaging agents.

METHODS

SPECT/CT and PET/CT with specific isotopes such as [68Ga]-1,4,7,10-tetra-azacyclododecane- N,N',N'',N'''-tetra-acetic acid (DOTA)-somatostatin analogs, [18F]-FDG and [18F]-fluorodopa have been clinically explored.

RESULTS

To overcome the limitations of SSTR imaging, interesting improvements are connected with the availability of new radiotracers, activating with different mechanisms compared to somatostatin analogues, such as glucagon-like peptide 1 receptor (GLP-1 R) agonists or antagonists.

CONCLUSION

This paper shows an overview of the RPs used so far in the imaging of pNETs with insight on potential new radiopharmaceuticals currently under clinical evaluation.

摘要

背景

神经内分泌肿瘤(NETs)是相对罕见的肿瘤,主要起源于消化系统,生长缓慢,常在发生转移时才被诊断出来。手术是唯一的治愈选择,但仅在少数患者中可行。其中,胰腺神经内分泌肿瘤(pNETs)占所有胰腺肿瘤的比例不到5%。可行的治疗选择包括生物疗法等药物治疗,以及最近的肽受体放射性核素疗法(PRRT),即使用放射性标记的生长抑素类似物。分子成像,主要是PET/CT,在pNETs患者中发挥着重要作用。

目的

利用NET中特定膜受体的过表达以及细胞摄取胺前体的能力,开发特异性靶向成像剂。

方法

已对使用诸如[68Ga]-1,4,7,10-四氮杂环十二烷-N,N',N'',N'''-四乙酸(DOTA)-生长抑素类似物、[18F]-FDG和[18F]-氟多巴等特定同位素的SPECT/CT和PET/CT进行了临床研究。

结果

为克服生长抑素受体(SSTR)成像的局限性,与新型放射性示踪剂的应用相关的有趣进展出现了,这些示踪剂通过与生长抑素类似物不同的机制激活,如胰高血糖素样肽1受体(GLP-1R)激动剂或拮抗剂。

结论

本文概述了目前在pNETs成像中使用的放射性药物,并深入探讨了目前正在临床评估的潜在新型放射性药物。

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